Plural Chalcogens Bonded Directly Patents (Class 544/240)
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Patent number: 5859008Abstract: Arylalkyl diazinone derivatives of the formula I ##STR1## and their physiologically acceptable salts, in whichR.sup.1, R.sup.2, R.sup.3, R.sup.4, B, Q and X have the meanings indicated in claim 1, exhibit phosphodiesterase IV inhibition and can be employed for the treatment of inflammatory processes and also of allergies, asthma and autoimmune disorders.Type: GrantFiled: September 13, 1996Date of Patent: January 12, 1999Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Rochus Jonas, Michael Wolf, Norbert Beier
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Patent number: 5821243Abstract: A compound of the formula: ##STR1## wherein R.sub.1 represents a lower alkyl (C.sub.1 --C.sub.6) substituent which may be straight or branched; R.sub.2 represents an aryl substituent of the formula: ##STR2## and Q, V, W, X, Y and Z are as set forth in the accompanying specification. These compounds are useful in prophylaxis and treatment of influenza virus infection.Type: GrantFiled: May 19, 1997Date of Patent: October 13, 1998Assignee: ViroPharma IncorporatedInventors: Guy D. Diana, Thomas R. Bailey, Theodore J. Nitz, Dorothy C. Young, William P. Gorczyca
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Patent number: 5795892Abstract: The invention concerns new 4-aminopyridazines of the general formula I ##STR1## in which R.sup.1 denotes an R.sup.2 --SO.sub.2 --O-- or R.sup.2 --SO.sub.2 --NR.sup.3 -- group in whichR.sup.2 denotes a cycloalkyl residue, an unsubstituted or substituted aryl or heteroaryl residue,R.sup.3 denotes a hydrogen atom, an alkyl or alkyloxyalkyl group which can be unsubstituted or substituted once or several times by hydroxy groups wherein the hydroxy groups can be substituted by alkyl, hydroxyalkyl, alkyloxyalkyl, hydroxyalkyloxyalkyl or alkylcarbonyl groups and wherein in each case two vicinal hydroxy groups can be linked together by alkylidene groups,as well as hydrates, solvates and physiologically tolerated salts thereof. The invention also concerns the optically active forms, racemates and mixtures of diastereomers of these compounds, processes for their production and pharmaceutical agents containing these compounds having a thrombin-inhibiting action.Type: GrantFiled: February 28, 1997Date of Patent: August 18, 1998Assignee: Boehringer Manneim GmbHInventors: Wolfgang Von Der Saal, Reinhard Heck, Ralf Kucznierz, Herbert Leinert, Karlheinz Stegmeier
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Patent number: 5763439Abstract: A pyridazinone derivative of the formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein Q, A, and R.sup.1 -R.sup.4 are as defined herein, useful as an anti-shock agent.Type: GrantFiled: March 4, 1996Date of Patent: June 9, 1998Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Itaru Shigehara, Shinji Odawara, Hiroshi Okada, Hirohiko Kimura, Masato Omatsu, Hitoshi Nakayama, Rie Higuchi, Taki Takenami
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Patent number: 5750523Abstract: Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: ##STR1## ?wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR.sup.1 (wherein R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or OR.sup.2 (wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group)}, is C.sub.1 -C.sub.8 alkylene wherein one carbon atom on the straight chain is substituted with one OR.sup.1 group (wherein R.sup.1 is the same as defined above), and Z.sup.1 and Z.sup.2 are independently a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a OR.sup.1 group (wherein R.sup.1 is the same as defined above)!.Type: GrantFiled: July 23, 1996Date of Patent: May 12, 1998Assignee: Nissan Chemical Industries, Ltd.Inventors: Keizo Tanikawa, Takashi Matsumoto, Hiroo Matsumoto, Nobutomo Tsuruzoe, Hitoshi Nakabeppu
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Patent number: 5728702Abstract: A 3(2H)-pyridazinone derivative of the formula (I) its salt, a process for its production and a pharmaceutical composition containing it. ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 which are independent of one another, is a hydrogen atom or a C.sub.1-4 alkyl group, X is a chlorine atom or a bromine atom, Y.sup.1 is a hydrogen atom, a halogen atom, a nitro group, an amino group or a C.sub.1-4 alkoxy group, Y.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, A is a C.sub.1-5 alkylene chain which may be substituted by a hydroxyl group, B is a carbonyl group or a methylene chain which may be substituted by a C.sub.1-4 alkyl group, and each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group, or R.sup.4 is a hydrogen atom and R.sup.5 is --Z--Ar (wherein Z is a C.sub.1-5 alkylene chain, and Ar is an aromatic 6-membered ring which may contain a nitrogen atom), or R.sup.4 and R.sup.5 together form a C.sub.Type: GrantFiled: March 22, 1996Date of Patent: March 17, 1998Assignee: Nissan Chemical Industries, Ltd.Inventors: Keizo Tanikawa, Akira Saito, Mitsuaki Hirotsuka, Ken-ichi Shikada
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Patent number: 5728699Abstract: The present invention presents a benzylsulfide derivative of the formula (I) or its salt: ##STR1## wherein R.sup.1 is a C.sub.1-6 alkyl group, a C.sub.1-6 haloalkyl group, a C.sub.2-4 alkenyl group, a cyano group, etc., and each of R.sup.2 and R.sup.3 is a hydrogen atom, a halogen atom, a cyano group, a C.sub.1-4 alkyl group, a C.sub.1-3 haloalkyl group, etc., R.sup.4 is a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group, etc., A is a hydrazinoaralkyl group or hydrazonoaralkyl group, and n is 0, 1 or 2; a process for its production; and a pesticide containing such a benzylsulfide derivative as an active ingredient. The benzylsulfide derivative of the present invention is capable of controlling various pests without adversely affecting crop plants.Type: GrantFiled: December 19, 1996Date of Patent: March 17, 1998Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Keiji Toriyabe, Hideharu Sasaki, Naoshi Masuyama, Akihide Nagai, Hiroyuki Yano, Mieko Kawashima, Yutaka Kurihara, Tomonori Shimazu
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Patent number: 5723411Abstract: Compounds of Formula I, and their N-oxides and agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein Q, W, R.sup.1, R.sup.2 and R.sup.3 are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective mount of a compound of Formula I.Type: GrantFiled: October 16, 1996Date of Patent: March 3, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Thomas Martin Stevenson
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Patent number: 5723460Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, wherein R.sup.1 is an optionally substituted alkyl group; X is --O--, --S--, or --N(R.sup.6), wherein R.sup.6 is a hydrogen atom or an optionally substituted alkyl group; R.sup.2 is an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or an optionally substituted alkyl, --CO.sub.2 R.sup.7 (wherein R.sup.7 is a hydrogen atom, am optionally substituted alkyl, aralkyl, aryl, aryloxyalkyl, alkanoyloxyalkyl or aroyloxyalkyl group), --CONR.sup.8 R.sup.9 (where R.sup.8 and R.sup.9, which may be the same or different, is as defined for R.sup.7), --CSNR.sup.8 R.sup.9, --CN or --CH.sub.2 CN group; Z is --(CH.sub.2).sub.n -- where n is zero or an integer 1, 2 or 3; R.sup.Type: GrantFiled: June 6, 1995Date of Patent: March 3, 1998Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, Valerie Anne Cole, Rikki Peter Alexander
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Patent number: 5719151Abstract: Phthalazinedione compounds and pharmaceutical compositions are described. The compositions are useful in treating human or animal patients to alleviate or cure disease or disease symptoms caused by nuclear ADP-ribosyl and similar transferases.Type: GrantFiled: January 13, 1995Date of Patent: February 17, 1998Inventors: Sydney Shall, Manoochehr Tavassoli
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Patent number: 5670504Abstract: A class of 2,6-diarylpyridazinones of general structural formula I have been identified that exhibit exhibit immunosuppressant activity with human T-lymphocytes, and are useful as an immunosuppressants.Type: GrantFiled: February 23, 1995Date of Patent: September 23, 1997Assignee: Merck & Co. Inc.Inventors: Richard J. Bochis, Andrew Kotliar, William H. Parsons, Kathleen Rupprecht
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Patent number: 5663402Abstract: There is disclosed a novel process for preparing products of the reaction of elemental phosphorus and elemental sulfur under reaction conditions wherein the phosphorus and sulfur are combined in a pre-mix at temperatures below the reaction temperature. The pre-mix may contain a diluent which is preferably the product of the reaction. Phosphorus pentasulfide can be prepared by heating the pre-mix to reaction temperatures wherein lower exotherm temperatures and reduced vibration are observed. Organophosphorus and thionated products can be prepared by the reaction of elemental sulfur and elemental phosphorus together with an organic compound wherein the ratio of phosphorus and sulfur generally corresponding to P.sub.2 S.sub.5. The process obviates the need for separately preparing phosphorus pentasulfide to prepare thiohated and organophosphorus compounds.Type: GrantFiled: March 27, 1995Date of Patent: September 2, 1997Assignee: G.D. Searle & CompanyInventors: Edward J. Griffith, Toan M. Ngo
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Patent number: 5659041Abstract: Radionuclide chelating compounds are provided for conjugation to targeting molecules such as proteins, peptides or antibodies. The resulting labeled targeting molecules may be used in diagnosis and therapy.Type: GrantFiled: September 2, 1994Date of Patent: August 19, 1997Assignee: Resolution Pharmaceuticals, Inc.Inventors: Alfred Pollak, Robert A. Kirby, Robert Dunn-Dufault
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Patent number: 5635494Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is CH.sub.3 --O-A.dbd.C--CO(V)CH.sub.3 ; n is 0 or 1;A is N or CH;V is O or NH;whereinY is O, S, NR.sub.1, or R.sub.6, the ring bond containing R.sub.4 and R.sub.5 is a single or double bond and R.sub.4 and R.sub.5 are independently selected from hydrogen and substituted or unsubstituted alkyl and aryl groups.Type: GrantFiled: April 21, 1995Date of Patent: June 3, 1997Assignee: Rohm and Haas CompanyInventors: Ronald Ross, Steven H. Shaber, Edward M. Szapacs
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Patent number: 5623072Abstract: Disclosed are certain 3-phenylpyridazines, compositions thereof which are herbicidal and methods of using such compositions for controlling undesired plants. Intermediates useful in preparing the 3-phenylpyridazines are disclosed.Type: GrantFiled: October 11, 1994Date of Patent: April 22, 1997Assignee: Monsanto CompanyInventors: Michael S. South, Terri L. Jakuboski
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Patent number: 5620993Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral fining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignee: Merck & Co., Inc.Inventors: Michael A. Patane, Mark G. Bock, Roger M. Friedinger
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Patent number: 5614633Abstract: Novel benzopyran and benzoxazine derivatives represented by the general formula: ##STR1## wherein R.sub.1 and R.sub.2 represent a lower haloalkyl group, R.sub.3 represents a hydrogen atom, etc., R.sub.4 represents a heterocyclic group or A--O-- wherein A represents a cyclic structure, etc., R.sub.5 and R.sub.6 represent a lower haloalkyl, X represents .dbd.N--, N.fwdarw.O, etc, are disclosed. These compounds exhibit K.sup.+ channel opening activating and can be widely used as an anti-asthma drug, an anti-epilepsy drug, etc.Type: GrantFiled: February 17, 1995Date of Patent: March 25, 1997Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Haruhiko Sato, Takenori Ishizawa, Hiroyuki Nabata
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Patent number: 5607624Abstract: A process for the preparation of compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, which comprises reacting a compound of formula III ##STR2## wherein the general symbols are as defined in claim 1, with a compound of formula IV[H].sub.n --R.sub.1 (IV).Type: GrantFiled: September 12, 1994Date of Patent: March 4, 1997Assignee: Ciba-Geigy CorporationInventors: Peter Nesvadba, Samuel Evans, Ralf Schmitt
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Patent number: 5604226Abstract: Pyridazinone derivatives of formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a methyl group which may be substituted with an aliphatic cyclic amino group optionally containing a hetero atom in the ring thereof; each of X.sup.1 and X.sup.2 independently represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, a cyano group, a nitro group or a group shown by --CO--NR.sup.2 R.sup.3 (wherein each of R.sup.2 and R.sup.3 independently represents an alkyl group having 1 to 6 carbon atoms); Y represents a halogen atom; Z represents an alkoxy group having 1 to 6 carbon atoms; l represents 0 or an integer of 1 to 3; A represents CH or N; m represents 0 or an integer of 1 or 2; and n represents an integer of 1 to 8, exhibit a platelet aggregation inhibiting activity and are useful for the treatment of circulatory disorders such as cerebral infarction.Type: GrantFiled: December 15, 1994Date of Patent: February 18, 1997Assignee: Nihon Nohyaku Co., Ltd.Inventors: Takashi Kagawa, Takuya Motokawa, Masanori Yoshida, Yoshitami Oshita, Kazuo Kanai
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Patent number: 5559080Abstract: Disclosed are certain 3-phenoxypyridazines, compositions thereof which are herbicidal and methods of using such compositions for controlling undesired plants. Intermediate compounds useful in preparing the phenoxypyridazines are also disclosed.Type: GrantFiled: October 11, 1994Date of Patent: September 24, 1996Assignee: Monsanto CompanyInventors: Michael S. South, Michael J. Miller
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Patent number: 5548078Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: December 20, 1994Date of Patent: August 20, 1996Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
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Patent number: 5527798Abstract: The invention provides a pyridazinone derivative having a high insecticidal and miticidal activity against agricultural noxious insects. The pyridazinone derivative of the invention is represented by the formula (1) ##STR1## wherein R is a hydrogen atom, an alkyl group, an alkoxyalkyl group, or a phenyl group which may have 1 or 2 substituents in an optional position.Type: GrantFiled: July 29, 1994Date of Patent: June 18, 1996Assignee: Otsuka Kaguku Kabushiki KaishaInventors: Isao Tada, Hisashi Takao
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Patent number: 5514679Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, hydroxy, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, alkylthioalkynyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy or cyanomethyl, nitro, difluoromethyl, trifluoromethyl or cyano;Y is alkylene of 3 to 9 carbon atoms;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkanoyl, alkanoyloxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, cyanomethyl, fluoroalkyl, cyano, phenyl, alkynyl, alkene, or halo;R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.Type: GrantFiled: May 13, 1994Date of Patent: May 7, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Theodore J. Nitz
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Patent number: 5506228Abstract: A class of 2,6-diarylpyridazinones of general structural formula I have been identified that exhibit exhibit immunosuppressant activity with human T-lymphocytes, and are useful as an immunosuppressants. ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form thereof, wherein:when M is S, R.sup.1 and R.sup.2 are selected from the following combinations:when R.sup.2 is 4-chloro, then R.sup.1 is 4-OCH.sub.3,2 -CH.sub.3, 4-Cl, 4-CH3,3-Cl, 3-CH3, 2-Cl, 4-H, 4-Br, 3-NO.sub.2 ; andwhen R.sup.2 is H, then R.sup.1 is 4-OCH.sub.3, andwhen M is --SO.sub.2 --, then R.sup.2 is H and R.sup.1 is 4-OCH.sub.3.As an immunosuppressant, these compounds are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.Type: GrantFiled: February 23, 1995Date of Patent: April 9, 1996Assignee: Merck & Co., Inc.Inventors: Richard Norton, Mohammed K. A. Ibraham
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Patent number: 5462914Abstract: Novel herbicidal N-cyanopyridazinones of the general formula ##STR1## in which the radicals R.sub.1, R.sub.2 and R.sub.3 independently of one another denote hydrogen, halogen, amino, nitro, cyano, alkyl, aryl, aralkyl, alkoxy or aryloxy groups, a process for their preparation, a herbicidal composition comprising them, and a method of controlling weeds.Type: GrantFiled: April 1, 1994Date of Patent: October 31, 1995Assignee: Sandoz Ltd.Inventors: Harald Leitner, Rudolf H. Worther, Horst Korntner, Rudolf Schneider, Engelbert Auer, Dietmar Kores, Hermann Tramberger
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Patent number: 5442062Abstract: The present invention provides a novel imidazole derivative having the chemical formula ##STR1## These compounds are useful for preventing or treating hypertension or congestive heart failure and have high activity, rapid action upon intravenous injection, good oral absorbtion, low toxicity, and long-lasting action. Also provided are pharmaceutical compositions which contain these compounds.Type: GrantFiled: April 22, 1994Date of Patent: August 15, 1995Assignee: The Upjohn CompanyInventors: Keiko Koh, Mikio Taniguchi, Noriie Itoh, Hiroshi Kushida, Osamu Morita, Hiroyoshi Yamada, Kiyotaka Munesada, Kazuo Tsuzuki, Mineo Kunihara, Yoshiji Fujita
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Patent number: 5439908Abstract: Compounds of the formula ##STR1## wherein A is a substituted or unsubstituted, aromatic or non-aromatic, monocyclic or bicyclic, heterocyclic radical that is bonded by way of a carbon atom to X; each of R.sub.1 and R.sub.2, independently of the other, is hydrogen or C.sub.1 -C.sub.6 alkyl; X is NR.sub.3, O or S; and R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: October 30, 1992Date of Patent: August 8, 1995Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna
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Patent number: 5434267Abstract: Process for the preparation of compounds of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X and n have the meaning given in the description, by reacting acetates with carbon monoxide in the presence of a basic auxiliary, followed by alkylation. The products are intermediates for fungicidal acrylates.Type: GrantFiled: March 14, 1994Date of Patent: July 18, 1995Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Alexander Klausener, Hans-Joachim Diehr
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Patent number: 5380718Abstract: Arthropodicidal tetrahydropyridazines of Formulae I and II, ##STR1## wherein Q,X,X.sup.1 Y, and G are as defined in the text, compositions containing them and their use in the control of arthropods.Type: GrantFiled: November 12, 1992Date of Patent: January 10, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventors: Charles R. Harrison, George P. Lahm, Thomas M. Stevenson
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Patent number: 5346902Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein Y is a specified small group or single atom and R.sup.1 and R.sup.2 are selected from a wide range of specified substituents.Type: GrantFiled: May 11, 1993Date of Patent: September 13, 1994Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine
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Patent number: 5292737Abstract: N,N'-Bis(sulfonamido)-2-amino-4-iminonaphthalen-1-ones and N,N'-Bis(amido)-2-amino-4-iminonaphthalen-1-ones are disclosed. Methods of inhibiting protein kinase C activity which comprises contacting protein kinase C with an effective amount of an N,N'-Bis(sulfonamido)-2-amino-4-iminonaphthalen-1-one or an N,N'-Bis(amido)-2-amino-4-iminonaphthalen-1-one are disclosed. Methods of treating an animal that is suspected of suffering from inflammatory, cardiovascular and/or neoplastic diseases which comprises administering an effective amount of an N,N'-Bis(sulfonamido)-2-amino-4-iminonaphthalen-1-one or an N,N'-Bis(amido)-2-amino-4-iminonaphthalen-1-one are disclosed.Type: GrantFiled: October 23, 1992Date of Patent: March 8, 1994Assignee: Sphinx Pharmaceuticals CorporationInventor: Jean M. Defauw
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Patent number: 5286725Abstract: There are described new pyridazinones endowed with acaricide and insecticide action, having general formula (I): ##STR1## wherein X is halo or alkyl, Z is alkylene and R is substituted cyclohexyl or cyclohexenyl.Type: GrantFiled: August 19, 1992Date of Patent: February 15, 1994Assignee: Ministero dell'Universita' e della Ricerca Scientifica e TechnologicaInventors: Franco Bettarini, Luigi Capuzzi, Sergio Massimini, Paolo Castoro, Vincenzo Caprioli
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Patent number: 5284971Abstract: Compounds of general formula (I) ##STR1## wherein R.sup.1 is (CH.sub.2).sub.n ((CHNR.sup.7 R.sup.8).sub.m C(O)R.sup.9 ; n=1-3; and m=0 or 1;R.sup.3 and R.sup.5 are independently Cl, Br, I, or CH.sub.3 ;R.sup.7 and R.sup.8 are independently H or (C.sub.1 -C.sub.4)alkyl;R.sup.9 is OH, (C.sub.1 -C.sub.4)alkoxy, or NR.sup.7 R.sup.8 ;R.sup.31 is H, Cl, Br, I, (C.sub.1 -C.sub.4)alkyl, (C.sub.4 -C.sub.6)cycloalkyl, (C.sub.1 -C.sub.4)haloalkyl, (C.sub.4 -C.sub.6)halocycloalkyl, or --CH(R.sup.10)Ar where Ar is selected from 5-hydroxypyrid-2-yl, 6-hydroxypyrid-3-yl, 6-hydroxypyridazin-3-yl, 6-methoxypyridazin-3-yl, 6-hydroxypyridazin-3-yl N-oxide, and 6-methoxypyridazin-3-yl N-oxide and R.sup.10 is H or (C.sub.1 -C.sub.4)alkyl;R.sup.41 is OH or a bioprecursor thereof; and the pharmaceutically acceptable salts thereof; are structural analogs of the thyroid hormones T.sub.3 and T.sub.4 and exhibit selective thyromimetic activity.Type: GrantFiled: July 16, 1992Date of Patent: February 8, 1994Assignee: Syntex (U.S.A.) Inc.Inventors: Keith A. Walker, Sharada S. Labadie, Denis J. Kertesz, Craig W. Laughton
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Patent number: 5278163Abstract: A novel 3(2H)-pyradazinone derivative of the formula (I) ##STR1## wherein, R represents an alkyl group having 1 to 4 carbon atoms substituted by a cycloalkyl group having 3 to 8 carbon atoms, an alkyl group having 1 to 4 carbon atoms substituted by a phenyl group which may be substituted or an alkyl group having 1 to 4 carbon atoms substituted by a heterocyclic group, R' represents a hydrogen atom, a halogen atom, an alkoxy group having 1 to 4 carbon atoms or a hydroxyl group having 1 to 4 carbon atoms, J represents any of various organic radicals. There is also provided a process for preparing said derivatives. These derivatives are useful as active ingredients of insecticidal, acaricidal and/or nematicidal compositions for agricultural and horticultural uses as well as of expellent compositions for pests parasitic on animals.Type: GrantFiled: October 5, 1992Date of Patent: January 11, 1994Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Yasuo Kawamura, Tatsuo Numata, Toshiyuki Umehara, Toshiro Miyake, Hiroshi Haruyama
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Patent number: 5254554Abstract: The application discloses pharmacologically-active 3-hydroxy-1-phenyl-1,4-dihydro-4-oxopyridazine compounds, derivatives thereof, a method for the preparation thereof, pharmaceutical compositions thereof, and a method of treating anxiety and other physiological abnormalities therewith.Type: GrantFiled: May 20, 1992Date of Patent: October 19, 1993Assignee: Pierre Fabre MedicamentInventors: Jean-Marie Autin, Dennis Bigg, Jean-Francois Patoiseau
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Patent number: 5245040Abstract: A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or a radical --CH.sub.2 B; A is an unsubstituted or mono- to tetrasubstituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, which may contain one or two substituents from the group comprising C.sub.1 -C.sub.3 haloalkyl having 1 to 7 halogen atoms, cyclopropyl, halocyclopropyl having 1 to 3 halogen atoms, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl and C.sub.2 -C.sub.3 haloalkynyl having 1 to 4 halogen atoms, C.sub.1 -C.sub.3 haloalkoxy having 1 to 7 halogen atoms, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkylthio having 1 to 7 halogen atoms, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro and one to four substituents from the group comprising C.sub.1 -C.sub.3 alkyl, C.sub.Type: GrantFiled: October 16, 1991Date of Patent: September 14, 1993Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Odd Kristiansen, Laurenz Gsell
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Patent number: 5202323Abstract: A compound of the formula, ##STR1## or its pharmaceutically acceptable salt, and its preparation process and pharmaceutical compositions characterized by containing these compounds as effective ingredients.These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic affections, congestive heart failure, hypertension, asthma, immediate type allergy diseases and the like.Type: GrantFiled: October 16, 1991Date of Patent: April 13, 1993Assignee: Nissan Chemical Industries Ltd.Inventors: Keizo Tanikawa, Akira Saito, Takashi Matsumoto, Ryozo Sakoda, Nobutomo Tsuruzoe, Ken-ichi Shikada
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Patent number: 5169848Abstract: Pyridazinones endowed with insecticidal and acaricidal activity are discld, which have the general formula: ##STR1## wherein the symbols have the meaning as defined in claim 1.Type: GrantFiled: April 4, 1990Date of Patent: December 8, 1992Assignee: Presidenza del Consiglio dei Ministri-Ufficio del Ministro per il coordinamento delle iniziative per la ricerva Scientifica e TecnologicaInventors: Franco Bettarini, Luigi Capuzzi, Sergio Massimini, Paolo Castoro, Vincenzo Caprioli
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Patent number: 5142048Abstract: The invention relates to novel intermediate compounds for preparation of novel amino acid derivatives having renin inhibiting activity.Type: GrantFiled: January 8, 1990Date of Patent: August 25, 1992Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Keiji Hemmi, Masahiro Neya, Hiroshi Marusawa, Keisuke Imai, Natsuko Kayakiri, Masashi Hashimoto
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Patent number: 5141939Abstract: Pesticidal substituted pyridazinones of the formula ##STR1## in which R.sup.1 represents alkyl, halogenolkyl, alkoxyalkyl, alkylthioalkyl, (di)alkylaminoalkyl, alkenyl or halogenoalkenyl, or represents in each case optionally substituted cycloalkyl, cycloalkylalkyl, aryl or aralkyl,R.sup.2 represents halogen or alkyl,R.sup.3 and R.sup.4 independently of one another in each case represent hydrogen or alkyl,R.sup.5 and R.sup.6 represent hydrogen, carboxyl, in each case optionally substituted straight-chain or branched alkyl, alkenyl, alkoxycarbonyl, aryl or aralkyl, or, together with the carbon atom to which they are bonded, rpresent an optionally substituted saturated or unsaturaated carbocyle,R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 independently of one another in each case represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio or halogenoalkylthio, andX represents oxygen or sulphur.Several intermediates therefor are also new.Type: GrantFiled: April 9, 1991Date of Patent: August 25, 1992Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel, Wolfgang Leicht
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Patent number: 5132307Abstract: New tetralin derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 and Z have the meanings indicated herein and salts thereof, exhibit an effect on the cardiovascular system.Type: GrantFiled: November 7, 1989Date of Patent: July 21, 1992Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Manfred Baumgarth, Rolf Gericke, Rolf Bergmann, Jacques De Peyer, Ingeborg Lues
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Patent number: 5110986Abstract: This application relates to a process for preparing a N-t-alkyl-1,2-diacylhydrazine by reacting a 1,3,4-oxadiazole with a tertiary alkyl cation precursor in the presence of a strong acid catalyst. Preferably, the 1,3,4-oxadiazole is a 2,5-disubstituted-1,3,4-oxadiazole and more preferably a 2,5-diaryl-1,3,4-oxadiazole. The strong acid catalyst is preferably a sulfur containing acid and more preferably sulfuric acid.Type: GrantFiled: April 26, 1988Date of Patent: May 5, 1992Assignee: Rohm and Haas CompanyInventor: Martha J. Kelly
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Patent number: 5103004Abstract: Heterocyclically substituted N-sultamsulfonamides, processes for their preparation and their use as herbicides and plant growth regulators.Compounds of the formula I or their salts ##STR1## wherein R.sup.1 and R.sup.2 denote H, halogen, alkyl, alkenyl, alkynyl or alkoxy, which can be substituted, or denote --(CH.sub.2).sub.n --COOR.sup.11 ;R.sup.3 denotes H, alkyl, alkenyl or alkynyl;R.sup.4 denotes a heterocyclic radical of the formulae ##STR2## where E is CH or N; X is O or S and a, b, c, d, e in each case denote 0, 1 or 2, with the proviso that c+d+e.gtoreq.2, possess excellent herbicidal and plant growth-regulating properties.Type: GrantFiled: August 23, 1991Date of Patent: April 7, 1992Assignee: Hoesch AktiengellschaftInventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 5086052Abstract: Pyridazinone, triazinone and oxapyridazinone compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.Type: GrantFiled: June 28, 1990Date of Patent: February 4, 1992Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, George W. Carter, Anwer Basha, Bruce P. Gunn, Richard D. Dyer
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Patent number: 5071860Abstract: Insecticidally active substituted heteroaryl phenyl ethers of the formula ##STR1## in which Het represents an optionally substituted heteroaromatic radical,X represents O, S, --CH.sub.2 --, --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.sub.2 --O--, ##STR2## Y represents O, --O--CH.sub.2 -- or S, Z represents an optionally substituted aromatic or heteroaromatic radical;m represents integers from 1-4n represents 0, 1, 2, 3, 4O represents 0, 1, 2, 3, 4, provided than n and o do not simultaneously represent 0p represents integers from 1-4,R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another represent hydrogen, C.sub.1 -C.sub.6 -alkyl which is optionally substituted; two radicals adjacent to one another can also, together with the C atoms to which they are bonded, form a saturated carbocyclic 5- or 6-ring,R.sup.1 represents identical or different radicals hydrogen, halogen, CN, C.sub.1-4 -alkyl, 1-5-halogeno-C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, 1-5-halogeno-C.sub.Type: GrantFiled: March 7, 1990Date of Patent: December 10, 1991Assignee: Bayer AktiengesellschaftInventors: Bernd Alig, Wilhelm Stendel, Michael Londershausen
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Patent number: 5070197Abstract: A method of preparing a water-soluble or water-dispersible pesticidal composition is described. The pesticidal composition is prepared in a continuous process by intimately mixing a Bronsted acid precursor of the pesticidally active compound with a Bronsted base under reaction conditions in an extruder. The reaction is performed with minimal solvent and under conditions where the water of reaction volatilizes during the course of the reaction.Type: GrantFiled: April 12, 1989Date of Patent: December 3, 1991Assignee: Uniroyal Chemical Company, Inc.Inventors: James Chin, James B. Marshall, Michael D. Drozdick, Fred C. Rosa, Frederick D. Judge
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Patent number: 5061798Abstract: This invention relates to chemical compounds which have selective thyromimetic activity. A compound of this invention is 3,5-dibromo-3'-[6-oxo-3)1H)-pyridazinylmethyl)-thyronine.Type: GrantFiled: October 27, 1989Date of Patent: October 29, 1991Assignee: Smith Kline & French Laboratories, Ltd.Inventors: John Colin Emmett, Paul D. Leeson
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Patent number: 5034388Abstract: This invention relates to derivatives of acrylic acid of the formula: ##STR1## useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of using them to combat fungi, especially fungal infections in plants. The values of the variables are provided herein.Type: GrantFiled: March 7, 1990Date of Patent: July 23, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey
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Pyridazinone derivatives, preparation thereof, and insecticidal, acaricidal, fungicidal compositions
Patent number: 5026850Abstract: Compounds of the formula: ##STR1## wherein R is a member selected from the group consisting of lower alkyls having from 2 to 4 carbon atoms; and chlorine and bromine. The compounds are useful as active ingredients in, e.g., insecticidal, acaricidal, nematicidal, fungicidal and expellant compositions.Type: GrantFiled: June 6, 1989Date of Patent: June 25, 1991Assignee: Nissan Chemical Industries, Ltd.Inventors: Masakazu Taniguchi, Masatoshi Baba, Yoshinori Ochiai, Masayoshi Hirose, Kiminori Hirata -
Patent number: 5011839Abstract: A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is hydrogen, 2-propenyl, or straight chained or branched C.sub.1 -C.sub.4 alkyl; each of R.sub.2 and R.sub.3 which may be the same or different, is hydrogen, or straight chained or branched C.sub.1 -C.sub.3 alkyl; X is chlorine, or bromine; Y is hydrogen, halogen, nitro, amino, or --AR.sub.4 wherein A is oxygen, or sulfur, and R.sub.4 is hydroen, straight chained, branched or cyclic C.sub.1 -C.sub.8 alkyl, ##STR2## wherein R.sub.5 is hydrogen, or straight chained or branched C.sub.1 -C.sub.4 alkyl; and Ar is ##STR3## wherein each Z.sub.1 and Z.sub.2 which may be the same or different, is hydrogen, halogen, straight or branched C.sub.1 -C.sub.4 alkyl, or --OR.sub.6 wherein R.sub.6 is straight or branched C.sub.1 -C.sub.4 alkyl, and B is oxygen, sulfur, or --N.dbd.C-- (to form a quinoline or pyridine ring); or a pharamaceutically acceptable salt thereof.Type: GrantFiled: December 4, 1989Date of Patent: April 30, 1991Assignee: Nissan Chemical Industries Ltd.Inventors: Keizo Tanikawa, Ryozo Saloda, Sakuya Tanaka, Kenichi Shikada